A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
C12Q 1/28 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase involving peroxidase
G01N 33/49 - Physical analysis of biological material of liquid biological material blood
G01N 33/493 - Physical analysis of biological material of liquid biological material urine
2.
COMBINATION OF MORPHINAN COMPOUNDS AND ANTIDEPRESSANT FOR THE TREATMENT OF PSEUDOBULBAR AFFECT, NEUROLOGICAL DISEASES, INTRACTABLE AND CHRONIC PAIN AND BRAIN INJURY
Provided herein are compositions comprising a dextromethorphan analog according to Formula I or Formula II or a pharmaceutically acceptable salt thereof of either of the foregoing, and a co-agent, e.g., an antidepressant such as a serotonin norepinephrine reuptake inhibitor; a serotonin noradrenaline dopamine reuptake inhibitor; a norepinephrine dopamine reuptake inhibitor; a monoamine oxidase inhibitor; a selective serotonin reuptake inhibitor; and a tricyclic antidepressant or a pharmaceutically acceptable salt of any of the foregoing. The compositions are useful in the treatment of pseudobulbar affect, neuropathic pain, neurodegenerative diseases, brain injuries, and the like.
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A method of treating a JAK-inhibition-responsive condition in a subject in need thereof, the method comprising: administering to the subject an effective amount of a compound represented by structural formulas (I) or (II), as described herein, or a pharmaceutically acceptable salt thereof.
A method of treating a JAK-inhibition-responsive condition (such as a hair loss disorder) in a human subject in need thereof, the method comprising administering to the human subject a therapeutically effective amount of Compound (I) or a pharmaceutically acceptable salt thereof, wherein each position designated specifically as deuterium has at least 95% incorporation of deuterium; and wherein: the subject is receiving a concomitant administration of a CYP3 A4 inhibitor; and the therapeutically effective amount of Compound (I), or a pharmaceutically acceptable salt thereof, is not reduced compared to the therapeutically effective amount of Compound (I), or pharmaceutically acceptable salt thereof, that would be administered to the subject in the absence of concomitant administration of a CYP3A4 inhibitor.
Certain aspects of the present invention are directed to improved processes for preparing enantiomerically enriched intermediates for the synthesis of ruxolitinib and deuterated forms of ruxolitinib. Certain aspects are also directed to deuterated intermediates useful in the synthesis of deuterated forms of ruxolitinib. Certain aspects are also directed to reaction mixtures for preparing enantiomerically enriched intermediates useful in the synthesis of ruxolitinib and deuterated forms of ruxolitinib.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
Disclosed is a JAK1 and/or JAK2 inhibitor of the following structural formula (I) or a pharmaceutically acceptable salt thereof. This invention also provides pharmaceutical compositions comprising a compound of Formula (I), optionally including additional therapeutic agents, and use in methods of treatment for hair loss disorders.
This disclosure relates to deuterated D-serine, pharmaceutically acceptable salts thereof, analogs and prodrugs thereof, pharmaceutical compositions thereof, and methods of use.
This disclosure relates to deuterated D-serine, pharmaceutically acceptable salts thereof, analogs and prodrugs thereof, pharmaceutical compositions thereof, and methods of use.
C07D 263/04 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07C 227/32 - Preparation of optical isomers by stereospecific synthesis
12.
PROCESS FOR PREPARING ENANTIOMERICALLY ENRICHED JAK INHIBITORS
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07B 59/00 - Introduction of isotopes of elements into organic compounds
Deuterated forms of volinanserin according to structural formula (I), and their pharmaceutically acceptable salts, pharmaceutical compositions containing these compounds, and methods of treatment or prevention using these compounds or pharmaceutical compositions are described. The compounds are useful for treating or preventing a disease or condition selected from psychosis, schizophrenia, schizoaffective disorder, Parkinson's disease, Lewy body dementia, sleep disorder (including insomnia), agitation, mood disorder (including depression), thromboembolic disorder, autism, and attention deficit hyperactivity disorder.
This invention also provides compound of Formula (I) including pharmaceutical compositions comprising a compound of Formula (I) and a pharmaceutically acceptable carrier. This invention also provides the use of such compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering pitolisant. Some exemplary embodiments include a method of treating a disease or condition selected from narcolepsy, daytime sleepiness (particularly in subjects suffering from Parkinson's disease or obstructive sleep apnea syndrome), and cognitive defects in psychiatric conditions, the method comprising the step of administering to a subject in need thereof a pharmaceutically acceptable composition of the present invention.
This disclosure relates to deuterated D-β-hydroxybutyric acid (DBHB) of Formula (I): wherein each of the variables are defined herein, and pharmaceutically acceptable salts thereof, analogs and prodrugs thereof, pharmaceutical compositions thereof, and methods of use.
A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
C07C 59/01 - Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
C07C 69/34 - Esters of acyclic saturated polycarboxylic acids having an esterified carboxyl group bound to an acyclic carbon atom
C07C 69/675 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids of saturated hydroxy-carboxylic acids
This disclosure relates to deuterated D-serine, pharmaceutically acceptable salts thereof, analogs and prodrugs thereof, pharmaceutical compositions thereof, and methods of use.
This invention relates to novel 2,3,6b,7,8,9,10,10a-octahydro-1H-pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalines, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a serotonergic, dopaminergic, and glutamatergic modulator.
This invention relates to deuterated forms of cenicriviroc, racemic and (R) forms thereof, free base forms of any of the foregoing and pharmaceutically acceptable salts of the free base forms. In one aspect, the invention provides a compound of Formula I:or a stereoisomer thereof, or a pharmaceutically acceptable salt of either of the foregoing, wherein each Y and each R is as defined in the application.
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
C07D 225/04 - Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
C07D 225/06 - Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with one six-membered ring
This invention relates to deuterated forms of hexahydro-4,7-methano-1H-isoindole-1,3(2H)-diones, and pharmaceutically acceptable salts thereof. In one aspect, the invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. This invention also provides compositions comprising a compound of this invention, including pharmaceutical compositions comprising the compound and a pharmaceutically acceptable carrier. This invention also provides the use of such compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a compounds that modulates the activity of a receptor selected from the group consisting of central dopamine Type 2 (D2) receptor and serotonin Type 2 (5HT2A) receptor. Some exemplary embodiments include a method of treating a disease or condition selected from schizophrenia and depressive episodes associated with bipolar I disorder, the method comprising the step of administering to a subject in need thereof a pharmaceutically acceptable composition of the present invention.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
This invention relates to indol-3-yl)ethyl]-3-(tetrafluoropropoxy)benzylamines of Formula (I), wherein each variable is defined herein, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an antagonist of the serotonin-6 (5-HT6) receptor, such as Alzheimer's Disease.
This invention relates to deuterated forms of miconazole and pharmaceutically acceptable salts thereof. This invention also provides pharmaceutical compositions comprising a compound of this invention and a pharmaceutically acceptable carrier. This invention also provides the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering miconazole, for example fungal infections and demyelination diseases.
A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
This invention relates to deuterated forms of venetoclax, and pharmaceutically acceptable salts thereof. Certain aspects of this invention also provide pharmaceutical compositions comprising a compound of the present invention and a pharmaceutically acceptable carrier. Certain aspects of the present invention also provide the use of such compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of the anti-apoptotic activity of the B-cell lymphoma 2 (Bcl-2) protein.
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
This invention relates to deuterated forms of bictegravir, and pharmaceutically acceptable salts thereof. In one aspect, the invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein each of Y1, Y2, Y3, Y4a, Y4b, Y5a, Y5b, Y6, Y7a, Y7b, Y8, Y9, Y10a, Y10b, Y11a, and Y11b is independently hydrogen or deuterium; provided that if each Y1, Y2, Y3, Y4a, Y4b, Y5a, Y5b, Y6, Y7a, Y7b, Y8, Y9, Y10a, Y10b, and Y11a is hydrogen, then Y11b is deuterium.
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/537 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
This invention relates to novel pyrrolo[2,3-b]pyridine compounds, and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted pyrrolo[2,3-b]pyridine compounds that are structurally related to fevipiprant. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a prostaglandin D2 receptor 2 antagonist (e.g., a CRTH2, GPR44, or PTGDR2 antagonist).
A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4353 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings
The invention is directed to compositions and combinations of compositions comprising one or more C-C motif chemokine receptor 5 (CCR5) antagonists, one or more checkpoint antagonists and/or one or more FAK antagonists and for use in inducing an immune response to diseases, such as cancer or for use in the production of a medicament or medicaments for use in inducing an immune response to diseases, such as cancer or to treat cancer. The invention also provides methods of treating cancer with a combination of antagonists. The antagonists may be administered sequentially or substantially simultaneously to effectively initiate, enable, increase, enhance, or prolong the activity and/or number of immune cells, or beneficial response to a tumor.
Disclosed is a method of treating in a subject hair loss disorders that are beneficially treated by administering a JAK1 and/or JAK2 inhibitor. The method comprises administering to the subject an amount in the range of about 4 mg to about 50 mg of Compound (I), or a pharmaceutically acceptable salt thereof. This invention also provides compositions comprising Compound (I) and the use of such compositions in the described methods.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/00 - Medicinal preparations containing organic active ingredients
This invention relates to novel deuterated forms of GFT-505, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are characterized by reduced PPAR- alpha and/or PPAR-delta activity.
This invention relates to deuterated forms of morpholinobenzo[d]thiazol-2-yl)-4-methylpiperidine-1-carboxamide compounds, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an adenosine A2A receptor antagonist.
A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
This invention relates to novel 2,3,6b,7,8,9,10,10a-octahydro-1H-pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalines, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a serotonergic, dopaminergic, and glutamatergic modulator.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
C07D 241/36 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
This invention relates to novel α-tocotrienol quinones of Formula I: (I), and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering Vitamin E.
This invention relates to methods of treating agitation comprising administering a morphinan compound or a pharmaceutically acceptable salt thereof. This invention also provides the use in methods of treating agitation and related disorders with such a morphinan compound in combination with quinidine, or pharmaceutically acceptable salt of either or both thereof.
This invention relates to methods of treating agitation comprising administering a morphinan compound or a pharmaceutically acceptable salt thereof. This invention also provides the use in methods of treating agitation and related disorders with such a morphinan compound in combination with quinidine, or a pharmaceutically acceptable salt of either or both thereof.
This invention relates to methods of treating agitation comprising administering a morphinan compound or a pharmaceutically acceptable salt thereof. This invention also provides the use in methods of treating agitation and related disorders with such a morphinan compound in combination with quinidine, or pharmaceutically acceptable salt of either or both thereof.
This invention relates to methods of treating agitation comprising administering a morphinan compound or a pharmaceutically acceptable salt thereof. This invention also provides the use in methods of treating agitation and related disorders with such a morphinan compound in combination with quinidine, or a pharmaceutically acceptable salt of either or both thereof.
This invention relates to deuterated forms of meclizine, and pharmaceutically acceptable salts or hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering meclizine and other Constitutive Androstane Receptor agonists or FGFR3 antagonists.
C07D 295/073 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
This invention relates to deuterated forms of filgotinib, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a JAK inhibitor.
This invention relates to novel thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepines, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of binding between an acetylated histone and a bromodomain-containing protein.
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
This invention relates to deuterated forms of obeticholic acid, and pharmaceutically acceptable salts thereof. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an agonist of the farnesoid X receptor (FXR).
A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
This invention relates to novel, deuterated forms of VX-661 and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating cystic fibrosis.
C07B 59/00 - Introduction of isotopes of elements into organic compounds
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
A61P 11/00 - Drugs for disorders of the respiratory system
This invention relates to novel 3-amido-4-oxo-5-phenoxypentanoic acids, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a caspase protease inhibitor.
C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
This invention relates to novel imidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one compounds, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions alone or in combination with other therapeutics in the treatment of diseases and conditions that are beneficially treated by administering an inducer of the gene encoding tumor necrosis factor (TNF) related apoptosis-inducing ligand (TRAIL) superfamily member 10.
This invention relates to novel, deuterated spiro-oxindole compounds of Formula I, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of reducing or eliminating pain and in treating diseases and conditions that are characterized by pain.
This invention relates to novel deuterated pyrimidinedione derivatives of Formula (I), and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating hepatitis C viral infections. The invention also provides novel intermediates useful in the synthesis of the compounds of the invention. Such intermediates may also have hepatitis C virus inhibitory properties.
This invention relates to novel substituted styryl benzylsulfones that are multikinase inhibitors and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an agent that inhibits kinases, such as phosphatidylinositol 3-kinase (PI3-K) and polo-like kinase (PLK-1).
C07C 317/10 - SulfonesSulfoxides having sulfone or sulfoxide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
A61K 31/136 - Amines, e.g. amantadine having aromatic rings, e.g. methadone having the amino group directly attached to the aromatic ring, e.g. benzeneamine
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
C07B 59/00 - Introduction of isotopes of elements into organic compounds
This invention relates to novel 4,4'-di(1H-imidazol-5-yl)-1,1'-biphenyl compounds, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an NS5A inhibitor.
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07B 59/00 - Introduction of isotopes of elements into organic compounds
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
This invention relates to novel phenyloxadiazole benzoic acids, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of premature translation termination and/or nonsense-mediated mRNA decay.
This invention relates to compounds of Formula (A), and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a viral DNA polymerase inhibitor.
This invention relates to novel inhibitors of the reuptake of one or more of serotonin, norepinephrine (also known as noradrenaline), or dopamine and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention, and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the reuptake of one or more of serotonin, norepinephrine, or dopamine.
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
C07C 237/10 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
This invention relates to deuterium substituted analogs of sacubitril and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering sacubitril. The invention also relates to compositions comprising a combination of a deuterated sacubitril analog and an angiotensin receptor antagonist. Such combinations are useful, for example, for treating patients with heart failure to reduce the risk of death from cardiovascular causes or hospitalization for heart failure.
C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
C07B 59/00 - Introduction of isotopes of elements into organic compounds
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
The present invention relates to a novel method of treating fibrotic disease in a patient. The method comprises administering to the patient an effective amount of compounds described herein and a galectin-3 inhibitor. This invention relates to a method of treating a fibrotic disease in a patient comprising administering to the patient an effective amount of a compound represented by the structural formula (I) or a pharmaceutically acceptable salt thereof, wherein one or more hydrogen atoms are optionally replaced with deuterium, and an effective amount of a galectin-3 inhibitor.
This invention relates to novel 3-phenylquinazolin-4-one compounds, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of phosphoinositide 3-kinase (PI3K).
The present invention relates to a novel method of treating chronic kidney disease in patient with macroalbuminuria. The method comprises administering to the patient an effective amount of a compound described herein.
The present invention relates to a novel method of treating hyperglycemia in a patient with poor glycemic control. The method comprises administering to the patient an effective amount of a compound described herein.
This invention relates to novel substituted triazolobenzodiazepines of the Formula (I), wherein each of the variables are defined herein and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering I-BET762.
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
The present invention in one embodiment provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula (I) are as defined in the specification.
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
Disclosed is a method of treating in a subject a disorder of the central nervous or pain. The method comprises administering to the subject an amount in the range of 2 mg/day to 60 mg/day of Compound (I) or a pharmaceutically acceptable salt thereof.
This invention relates to novel substituted styryl benzylsulfones that are multikinase inhibitors and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an agent that inhibits kinases, such as phosphatidylinositol 3-kinase (PI3-K) and polo-like kinase (PLK-1).
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/136 - Amines, e.g. amantadine having aromatic rings, e.g. methadone having the amino group directly attached to the aromatic ring, e.g. benzeneamine
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
59.
DEUTERATED DERIVATIVES OF A THIENOTRIAZOLODIAZAPINE BROMODOMAIN-CONTAINING PROTEIN INHIBITOR
The present invention in one embodiment provides a compound of Formula I: (I), or a pharmaceutically acceptable salt thereof, wherein Y1, Y2 and Y3 are each independently selected from hydrogen and deuterium; R1, R2, and R3 are each methyl and are independently substituted with 0 to 3 deuterium; and R4 is t-butyl and is substituted with 0 to 9 deuterium; provided that if R1, R2 and R3 are each -CH3, and R4 is -C(CH3)3, then at least one of Y1 and Y2 is deuterium.
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
60.
DEUTERATED INTEDANIB DERIVATIVES AND THEIR USE FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
The present invention provides a deuterated compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula I are as defined in the specification. The compound of Formula I is useful for the treatment of cancer such as non-small cell lung cancer, ovarian cancer, renal cell carcinoma, hepatocellular carcinoma, and glioblastoma multiforme, and/or fibrosis, such as pulmonary fibrosis, including IPF.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07B 59/00 - Introduction of isotopes of elements into organic compounds
The present invention in one embodiment provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula I are as defined in the specification.
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
63.
INHIBITORS OF THE ENZYME UDP-GLUCOSE: N-ACYL-SPHINGOSINE GLUCOSYLTRANSFERASE
This invention relates to novel inhibitors of UDP-glucose: N-acyl-sphingosine glucosyltransferase and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of UDP-glucose: N-acyl-sphingosine glucosyltransferase.
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
This invention relates to novel inhibitors of the reuptake of one or more of serotonin, norepinephrine, or dopamine and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the reuptake of one or more of serotonin, norepinephrine, or dopamine.
This invention relates to novel pyrido[2,3-d]pyrimidinones and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CDK-4 and/or CDK-6 inhibitor.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
This invention relates to novel NS5B polymerase inhibitors and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of HCV.
C07B 59/00 - Introduction of isotopes of elements into organic compounds
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
The present invention in one embodiment provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula I are as defined in the specification.
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
This invention relates to novel substituted dioxopiperidinyl phthalimide derivatives and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an immunomodulatory agent.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
This invention relates to novel ALK inhibitors of Formula I: as defined in the specification, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering ALK inhibitors.
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
This invention relates to novel fluoro-derivatives of pyrazole-substituted amino-heteroaryl compounds of Formula (I):, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of anaplastic lymphoma kinase (ALK).
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
This invention relates to deuterated compounds of Formula I and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.
C07D 215/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
The invention in one embodiment is directed to solid forms of { S-3-(4- Amino- 1 -oxo- isoindolin-2-yl)(piperidine-3,4,4,5,5-d5)-2,6-dione}, including an anhydrous crystalline form, two hydrates, and an amorphous form. The invention in one embodiment is directed to methods of preparation of the solid forms.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
C07C 69/24 - Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with monohydroxylic compounds
C07C 59/01 - Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
C07B 59/00 - Introduction of isotopes of elements into organic compounds
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
The present invention in one embodiment provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula I are as defined in the specification.
The present invention in one embodiment provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula (I) are as defined in the specification.
The present invention in one embodiment provides a compound of Formula 1 (structurally represented), or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula I are as defined in the specification. The compound of Formula I is useful for the treatment of diseases such as a disease selected from the group consisting of multiple myeloma, solid tumors, lymphoma, and leukemia.
A61K 31/175 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine having the group , N—C(O)—N=N— or , e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazonesThioanalogues thereof
The present invention in one embodiment provides a compound of Formula I:(I), or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula I are as defined in the specification.
The present invention in one embodiment provides a compound of Formula I: Formula I, or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula I are as defined in the specification. The compound of Formula I is useful for the treatment of a disease selected from the group consisting of inflammatory bowel disease (IBD), such as Crohn's disease or ulcerative colitis, and celiac disease.
This invention relates to novel pyrazole-substituted amino-heteroaryl compounds of Formula (I) and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of anaplastic lymphoma kinase (ALK).
The present invention in one embodiment provides a compound of Formula A: or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising the compound; and methods of treating the indications disclosed herein.
The present invention provides the Form 2 crystalline polymorph of 7-(ieri-Butyl-d9)-3- (2,5-difluorophenyl)-6-((1-methyl-lH-l,2,4-triazol-5-yl)methoxy)-[l,2,4]triazolo[4,3- b]pyridazine. The polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data ("XRPD"); (b) differential scanning calorimetry ("DSC"); (c) FT- Raman spectrum; (d) FT-IT spectrum; and (e) thermogravimetric analysis (TGA).
The present invention provides individual crystalline polymorphs of 7-(tert-Butyl-d9)-3-(2,5-difluorophenyl)-6-((1-methyl-1H-1,2,4- triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine designated Form 1, Form 3 and Form 4. Each polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data ("XRPD"); (b) differential scanning calorimetry ("DSC"); and (e) thermogravimetric analysis (TGA).
The present invention provides individual crystalline polymorphs of 7-(tert-Butyl- d9)-3-(2,5-difluorophenyl)-6-((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)- [1,2,4]triazolo[4,3-b]pyridazine designated Form 5. The Form 5 polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data ("XRPD"); (b) differential scanning calorimetry ("DSC"); (c) FT-Raman spectroscopy; (d) FT-IR spectroscopy; and (e) thermogravimetric analysis (TGA).
The present invention provides in one embodiment individual crystalline polymorphs of (S)-1-(4,4,6,6,6-pentadeutero-5-hydroxyhexyl)-3,7-dimethyl-1H-purine- 2,6(3H,7H)-dione designated Form 1, Form 2, Form 3 and Form 4. Each polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data ("XRPD"); (b) differential scanning calorimetry ("DSC"); and (e) thermogravimetric analysis (TGA).
C07D 473/04 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
This invention relates to novel substituted styryl benzylsulfones that are multikinase inhibitors and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an agent that inhibits kinases, such as phosphatidylinositol 3- kinase (PI3-K) and polo-like kinase (PLK-1).
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentifylline and related compounds are beneficial.
This invention relates to novel substituted dioxopiperidinyl phthalimide derivatives and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an immunomodulatory agent.
C07D 211/02 - Preparation by ring-closure or hydrogenation
C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07C 275/16 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton being further substituted by carboxyl groups
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C07D 211/88 - Oxygen atoms attached in positions 2 and 6, e.g. glutarimide
This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of a phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol.
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: [Insert Formulas B, A, I, C, and E] as described herein. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a selective T-type calcium channel blocker.
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
(1) Pharmaceutical preparations for the treatment of diabetic nephropathy, multiple myeloma, and spasticity; pharmaceutical preparations for the relief of pain, pelvic inflammatory disease, and inflammatory connective tissue diseases; pharmaceutical preparations for the treatment of respiratory diseases, namely, chronic obstructive pulmonary disease; pharmaceutical preparations for the treatment of genetic diseases, namely, cystic fibrosis; pharmaceutical preparations for the treatment of renal diseases, namely, diabetic nephropathy; pharmaceutical preparations for the treatment of sleep disorders, namely, excess daytime sleepiness in narcolepsy and cataplexy in narcolepsy; pharmaceutical preparations for the treatment of agitation in Alzheimer's disease, major depressive disorder, and schizophrenia; pharmaceutical preparations for the treatment of psoriasis and psoriatic arthritis.
(2) Prescription pharmaceutical and biopharmaceutical preparations, namely, preparations for the treatment of inflammatory diseases, namely, inflammatory bowel diseases, pelvic inflammatory diseases, inflammatory connective tissue diseases (1) Pharmaceutical research and development services
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical preparations; biopharmaceutical preparations; pharmaceutical and biopharmaceutical preparations for veterinary use; pharmaceutical preparations for the treatment of the central nervous system, namely, central nervous system infections, brain diseases, mood disorders, cognitive disorders, anxiety disorders, alcoholism, central nervous system movement disorders, ocular motility disorders, narcolepsy, pseudo bulbar affect, nerve compression syndromes, neuritis, neuralgia and regional pain syndromes, insomnia, bipolar disorder, seizure disorders; pharmaceutical preparations for the treatments of smoking cessation, encephalitis, cerebral palsy, Parkinson's disease, Huntington's disease, fibromyalgia and spinal cord diseases, cancer and cardiovascular disease; pharmaceutical preparations for the treatment of inflammatory diseases, namely, inflammatory bowel diseases, diabetic nephropathy, multiple myeloma, HIV, spasticity; pharmaceutical preparations for the relief of pain, pelvic inflammatory disease, inflammatory connective tissue diseases; none of the aforesaid preparations being for the treatment of central nervous system diseases and disorders, namely, attention deficit hyperactivity disorder and/or attention deficit disorder either alone or with related disorders. Research and development in the pharmaceutical and biotechnology fields; clinical testing of pharmaceuticals; providing medical and scientific research information in the field of pharmaceuticals and clinical trials.
The present invention in one embodiment relates to a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein: each of R1 and R2 is independently selected from -CH3 and -CD3; R3 is hydrogen or deuterium; each of Z1, Z2 and Z3 is independently selected from hydrogen and deuterium; each Z4 is hydrogen or deuterium; each Z5 is hydrogen or deuterium; and each Z6 is hydrogen or deuterium.
C07D 473/04 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
The present invention provides a compound of Formula (I) or (II) or a pharmaceutically acceptable salt of any of the foregoing, wherein each of the variables is as defined herein. The compounds of the invention can be used in therapy, for example, to improve the efficacy of a therapeutic agent that is either (i) metabolized by a liver metabolic enzyme; (ii) transported by an efflux pump; or (iii) a combination of (i) and (ii), especially a HCV protease inhibitor or a HIV protease inhibitor.
C07D 213/04 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.
C07D 215/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
C07B 59/00 - Introduction of isotopes of elements into organic compounds
C07C 311/39 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
This invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an HIV integrase inhibitor.
A61K 31/5365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
